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Ibufenac (Synonyms: Dytransin,Ibunac,4-Isobutylphenylacetic Acid,NSC 99976)

Catalog No.GC18010

COX-1 and -2 inhibitor

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Ibufenac Chemical Structure

Cas No.: 1553-60-2

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Sample solution is provided at 25 µL, 10mM.

Description of Ibufenac

IC50: 17.4 and 13.1 μM for COX-1 and -2, respectively.

Ibufenac is a dual COX-1 and -2 inhibitor.

Cyclooxygenase (COX), also known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme that is responsible for formation of prostanoids, such as thromboxane and prostaglandins.

In vitro: Ibufenac was identified as an analog of the NSAID ibuprofen that could inhibit COX-1 and -2 activity with IC50 values of 17.4 and 13.1 μM, respectively [1].

In vivo: In a previous animal study, two new structural analogs, R3 and R4, along with their parent compounds, ibufenac and ibuprofen, were evaluated for their biopharmaceutical properties. Aanti-inflammatory activity was evaluated by topically administering drugs to inhibit inflammation induced by using either clove oil or arachidonic acid. Results showed that the rank order of activity was ibufenac approximately equal to ibuprofen > R3 approximately equal to R4 [2].

Clinical trial: Early clinical study found that ibufenac was a useful drug in the treatment of the symptoms of rheumatoid arthritis. Ibufenac appeared to be as effective as aspirin in this respect at the dosage levels applied and its usage was associated with considerably fewer side effects [3].

References:
[1] Gülcan, H. O.,nlü, S.,Dimoglo, A., et al. Marginally designed new profen analogues have the potential to inhibit cyclooxygenase enzymes. Arch.Pharm.Chem.Life Sci. 348, 55-61 (2015).
[2] Rao CS, Schoenwald RD, Barfknecht CF, Laban SL.  Biopharmaceutical evaluation of ibufenac, ibuprofen, and their hydroxyethoxy analogs in the rabbit eye. J Pharmacokinet Biopharm. 1992 Aug;20(4):357-88.
[3] T.  M. Chalmers. Clinical Trials of a New Drug, Ibufenac, in the Treatment of Rheumatoid Arthritis Ann Rheum Dis. 1963 Sep; 22(5): 358–362.

Chemical Properties of Ibufenac

Cas No. 1553-60-2 SDF
Synonyms Dytransin,Ibunac,4-Isobutylphenylacetic Acid,NSC 99976
Chemical Name 4-(2-methylpropyl)-benzeneacetic acid
Canonical SMILES CC(C)CC1=CC=C(CC(O)=O)C=C1
Formula C12H16O2 M.Wt 192.3
Solubility ≥ 6.9mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Ibufenac

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1 mg 5 mg 10 mg
1 mM 5.2002 mL 26.001 mL 52.0021 mL
5 mM 1.04 mL 5.2002 mL 10.4004 mL
10 mM 0.52 mL 2.6001 mL 5.2002 mL
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In vivo Formulation Calculator (Clear solution) of Ibufenac

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 25 reference(s) in Google Scholar.)

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